CN107349192A - Poria cocos skin zone extract, Poria cocos eo-acid A and Poria cocos eo-acid B are in the purposes of regulation blood glucose - Google Patents
Poria cocos skin zone extract, Poria cocos eo-acid A and Poria cocos eo-acid B are in the purposes of regulation blood glucose Download PDFInfo
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- CN107349192A CN107349192A CN201710320602.9A CN201710320602A CN107349192A CN 107349192 A CN107349192 A CN 107349192A CN 201710320602 A CN201710320602 A CN 201710320602A CN 107349192 A CN107349192 A CN 107349192A
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- 208000019622 heart disease Diseases 0.000 description 1
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- 201000001881 impotence Diseases 0.000 description 1
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- 229940021222 peritoneal dialysis isotonic solution Drugs 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/42—Separation; Purification; Stabilisation; Use of additives
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L31/00—Edible extracts or preparations of fungi; Preparation or treatment thereof
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/06—Fungi, e.g. yeasts
- A61K36/07—Basidiomycota, e.g. Cryptococcus
- A61K36/076—Poria
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
- C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
- C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
- C07C2603/16—Benz[e]indenes; Hydrogenated benz[e]indenes
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Abstract
Poria cocos skin zone extract, Poria cocos eo-acid A and Poria cocos eo-acid B are in the purposes of regulation blood glucose.One kind is used to adjust blood glucose using at least one of Poria cocos eo-acid A (poricoic acid A) and Poria cocos eo-acid B (poricoic acid B) in the purposes for preparing a medicine or a food, wherein medicine or food.At least one of Poria cocos eo-acid A and Poria cocos eo-acid B can be used in the form of plant extract, wherein with the gross weight meter of the plant extract, the total content of Poria cocos eo-acid A and Poria cocos eo-acid B in the plant extract are not less than 30 weight %.The food can be health food, nutrient supplement food or food of special nutrients.
Description
Technical field
The present invention is on Poria cocos skin zone extract, Poria cocos eo-acid A (poricoic acid A) and Poria cocos eo-acid B
The application of (poricoic acid B), especially with respect to these materials in the application of regulation blood glucose.
Background technology
Diabetes are a kind of chronic metabolic disorder diseases, and its Etiological is that organism inner cell absorbs glucose
Mechanism operation makes Glucose in Blood by Cyclic too high extremely.In general, the insulin secreted by the β cells of pancreas can stimulate fat
Fat cell and muscle cell intake glucose, have the effect of regulation blood glucose.When organism is made due to factors such as obesity, agings
In adult amount of insulin secretion deficiency or to insulin sensitivity it is bad when, blood sugar concentration can raise.Hyperglycaemia may result in
Such as the complication such as hypertension, heart disease, artery sclerosis, high fat of blood, blindness, impotence more occur when serious, amputation, washes kidney etc.
Sequelae.
Clinically mainly include the modes such as motion, diet control and drug therapy for the therapeutic modality of diabetes at present,
Its drug treatment includes injection of insulin, oral hypoglycaemic medicine, such as sulphonyl urea class medicine (sufonylureas), double
Guanidine medicine (biguanides), alpha-glucosidase restrainer (alpha-glucosidase inhibitors), insulin
Sensitizer (insulin sensitizer) etc..However, with human lives' morphologic change, the prevalence rate of diabetes also increases year by year
Add.According to the prediction of the World Health Organization in 2008, it is contemplated that in the year two thousand thirty, global diabetes population will more than 300,000,000 people, therefore,
Industry be still directed to develop side effect it is low and can be effectively hypoglycemic medicine or method.
Present inventor, which studies, to be found, Poria cocos skin zone extract and its contained Poria cocos eo-acid A (poricoic acid
A) and Poria cocos eo-acid B (poricoic acid B), the ability of cellular uptake glucose all can be effectively lifted, therefore available for adjusting
Blood glucose, it is provided in particular in excellent effect of lowering blood sugar.
The content of the invention
One object of the present invention, it is to provide a kind of using at least one in manufacture of Poria cocos eo-acid A and Poria cocos eo-acid B
The purposes of one medicine or food, the wherein medicine or food are used to adjust blood glucose.With Poria cocos eo-acid A and Poria cocos eo-acid B gross weight
The dosage of gauge, the medicine or food be daily about 0.05 mg kg of body weight to 1 mg kg of body weight, and the food can be with
For health food, nutrient supplement food or food of special nutrients.
It is preferred that at least one of Poria cocos eo-acid A and Poria cocos eo-acid B is used in the form of plant extract.In the plant
In extract, with the gross weight meter of plant extract, Poria cocos eo-acid A and Poria cocos eo-acid B total content are not less than 30 weight %, compared with
It is good to be not less than 40 weight %.More preferably, Poria cocos eo-acid A's and Poria cocos eo-acid B is at least one in the form of Poria cocos skin zone extract
Use.In the Poria cocos skin zone extract, with the gross weight meter of Poria cocos skin zone extract, pachymic acid (pachymic acid), go
Hydrogen pachymic acid (dehydropachymic acid), soil not sour (tumulosic acid) and dehydrotumulosic acid
Each content of (dehydrotumulosic acid) is all no more than 0.5 weight %, and dehydrogenation bolt bacterium acid
(dehydrotrametenolic acid), bolt bacterium acid (trametenolic acid), dehydrogenation shelf fungus acid
Each content of (dehydroeburicoic acid), shelf fungus acid (eburicoic acid) is all no more than 5%.It is preferred that
In the Poria cocos skin zone extract, with the gross weight meter of Poria cocos skin zone extract, dehydrogenation bolt bacterium acid, bolt bacterium acid, dehydrogenation shelf fungus
Acid, each content of shelf fungus acid are all no more than 2.5%.More preferably, in the Poria cocos skin zone extract, extracted with Poria cocos skin zone
The gross weight meter of thing, dehydrogenation bolt bacterium acid, bolt bacterium acid, dehydrogenation shelf fungus acid, each content of shelf fungus acid are all no more than 1%.
Another object of the present invention, in providing a kind of method that blood glucose is adjusted in an individual, it is included to one
Individual in need applies at least one of the Poria cocos eo-acid A and Poria cocos eo-acid B of an effective dose.
Another object of the present invention, it is to provide a kind of composition for adjusting blood glucose, said composition is a medicine or food
Product, and the Poria cocos eo-acid A's comprising an effective dose and Poria cocos eo-acid B is at least one.
Preferably, the Poria cocos skin zone extract is provided with the operation comprised the following steps：
(a) with the Poria cocos skin zone of one first solvent extraction one, obtain one and slightly extract thing；
(b) the thick extraction thing is dried, one is obtained and slightly extracts thing powder；
(c) thick extraction thing powder with one second solvent extraction, obtains a Poria cocos skin zone extract,
Wherein, first solvent is identical or different with second solvent and is respectively selected from water, ethanol, alkali lye, acid solution and preceding
The combination stated.
Wherein, first solvent and the second solvent are that concentration of alcohol is identical or different ethanol water.
The beneficial effects of the invention are as follows：Poria cocos skin zone of the present invention extract and Poria cocos eo-acid A and Poria cocos eo-acid B really may be used
The ability of biological cell intake blood glucose is lifted, available for adjusting blood glucose, and especially can reduce too high blood glucose.
Brief description of the drawings
The present invention is further detailed explanation with reference to the accompanying drawings and detailed description.
Fig. 1 is shown to be detected with the glycoxidative ferment method of grape (glucose oxidase assay), Poria cocos skin zone extract
To the result of the influence of glucose ability in mouse muscle cellular uptake nutrient solution；
Fig. 2, which is shown, to be absorbed to mouse adipocytes and is cultivated with the glycoxidative ferment method detection of grape, Poria cocos skin zone extract
The result of the influence of glucose ability in liquid；
Fig. 3 A are shown with the glycoxidative ferment method detection of grape, and Poria cocos eo-acid A is in mouse muscle cellular uptake nutrient solution
The result of the influence of glucose ability；
Fig. 3 B are shown with the glycoxidative ferment method detection of grape, and Poria cocos eo-acid B is in mouse muscle cellular uptake nutrient solution
The result of the influence of glucose ability；
Fig. 4 A are shown to be absorbed in nutrient solution with the glycoxidative ferment method detection of grape, Poria cocos eo-acid A to mouse adipocytes
The result of the influence of glucose ability；
Fig. 4 B are shown to be absorbed in nutrient solution with the glycoxidative ferment method detection of grape, Poria cocos eo-acid B to mouse adipocytes
The result of the influence of glucose ability.
Embodiment
Some embodiments of the invention explained below；But under without departing substantially from spirit of the invention, the present invention may be used also
State in many different forms is put into practice, and the scope of the present invention should not be considered limited to the content that specification is stated.
In addition, unless Wen Zhongyou illustrates in addition, in this specification (especially in detail in the claims) used in " one ", "the" and
Similar term is interpreted as including odd number and plural form；So-called " effective dose ", when referring to administering to individual, it can effectively lift this
The compound amounts of the ability of the cellular uptake glucose of body；So-called " individual " refers to mammal, mammal can be the mankind or
Non-human animal；So-called " regulation blood glucose " refers to towards the direction of normal value and changes the concentration of glucose in blood；Unit " mg/kg body
Weight " refers to the needed dosage of per kilogram of body weight individual.
Number range (such as 5 to 100) as used in this specification is interpreted as being also contained in all in the scope
The scope that rational and any rational in this range are formed, therefore, number range as used in this specification
It is possible to combine comprising the numerical value between cited minimum and peak.In addition, make when herein before numerical value
During with " about ", substantially represent and differed with the numerical value within 20%, preferably within 10%, and more preferably within 5%.
As described above, the Etiological of diabetes is that the mechanism operation of organism inner cell intake glucose makes blood extremely
Glucose content in liquid is too high.Present inventor, which studies, to be found, Poria cocos eo-acid A and Poria cocos eo-acid B can all lift cell and take the photograph
The ability of glucose is taken, therefore available for blood glucose is adjusted, especially reduce too high blood glucose.Therefore, the present invention provides one kind and made
With Poria cocos eo-acid A and Poria cocos eo-acid B it is at least one in regulation blood glucose application, including the use of Poria cocos eo-acid A and Poria cocos eo-acid B
It is at least one in prepare one regulation blood glucose medicine or food, to it is in need individual administering Poria cocos eo-acid A and Poria cocos eo-acid B
It is at least one with adjust the method for blood glucose and provide one include Poria cocos eo-acid A and Poria cocos eo-acid B at least one food
Or medical composition.
Poria cocos medicinal material refers to the dry sclerotia for intending shelf fungus section fungi (Poria cocos (Schw.) Wolf).Poria cocos fungi
Often colonize on pine roots, crust is in light brown or dark brown (Poria cocos skin zone), internal then pinkiness or white (Poria cocos meat
Portion).Traditional Chinese Medicine ancient books and records are recorded, and Poria cocos meat portion has calmness, diuresis, extra-nutrition, strengthen immunity and postpones the use such as aging
On the way, and Poria cocos skin zone be only applied to treat hydroderma.
As shown in rear attached embodiment, according to the present invention, it can obtain a Poria cocos eo-acid A's and Poria cocos eo-acid B by Poria cocos skin zone
Total content is not less than 30 weight % (with the gross weight meter of Poria cocos skin zone extract) Poria cocos skin zone extract.Therefore, according to this
Used by invention Poria cocos eo-acid A and Poria cocos eo-acid B it is at least one can such as Poria cocos skin zone extract plant extract
Form use, it is new with the gross weight meter of plant extract, Poria cocos wherein in according in plant extract of the present invention
Sour A and Poria cocos eo-acid B total content is not less than 30 weight %, is preferably not less than 40 weight %.
According to the present invention, the operation that used Poria cocos skin zone extract can be one to comprise the following steps is provided
Extract：(a) with one first polar solvent extract Poria cocos skin zone, obtain one and slightly extract thing；(b) the thick extraction thing is dried, it is thick to obtain one
Extract thing powder；(c) with one second polar solvent extract this it is thick extraction thing powder, obtain a Poria cocos skin zone extract, wherein this first
Polar solvent is identical or different with second polar solvent and is respectively selected from water, ethanol, alkali lye, acid solution and foregoing combination.Its
In, alkali lye refer to any suitable pH value more than 7 alkaline solution (such as：Sodium hydroxide solution), and acid solution refer to it is any suitable
PH value less than 7 acid solution (such as：Hydrochloric acid solution).In the section Example of the present invention, concentration of alcohol is used to be identical
Or different ethanol waters is as the first polar solvent and the second polar solvent.
In step (a), the dosage ratio of the first polar solvent and Poria cocos skin zone can be optionally adjusted.In general, the
The dosage of one polar solvent have no it is specifically limited, as long as raw material can be made dispersed.For example, can be adopted in step (a)
Volume ratio with the first polar solvent and Poria cocos skin zone is about 8：1 to about 16：1 dosage.In a specific embodiment of the invention,
Using ethanol water as the first polar solvent, and with volume ratio about 1：8 Poria cocos skin zone：Ethanol water carries out step (a)
Extraction.
In step (a), it is visual used by the first polar solvent select suitable extraction time.With using ethanol water
Solution is as the first polar solvent and Poria cocos skin zone：The volume ratio of ethanol water is 1：Exemplified by 8, generally extraction lasts at least 1
Hour, preferably at least 2 hours, more preferably at least 3 hours.In addition, can optionally be aided with for example decoct, cool down, filtering, depressurize it is dense
Contracting, resin col-umn chromatography etc. are other to be operated to carry out step (a).In addition, before can be if necessary in progress step (a), first by Fu
Siberian cocklebur skin zone pre-soaking a period of time in the first polar solvent., can be first to use ethanol water exemplified by the first polar solvent
Carry out pre-soaking about 12 hours.
In step (c), the second polar solvent and the use of the thick extraction thing powder obtained by step (b) can be optionally adjusted
Amount ratio.In general, the dosage of the second polar solvent have no it is specifically limited, as long as can make slightly to extract thing powder dispersed.
For example, in step (c) the second polar solvent can be used slightly to extract the volume ratio of thing powder with Poria cocos skin zone as about 8：1 to about
16：1 dosage.In a specific embodiment of the invention, using ethanol water as the second polar solvent, and using volume ratio as about 1：
8 Poria cocos skin zone slightly extracts thing powder：Ethanol water carries out the extraction of step (c).
According to Poria cocos skin zone of the present invention extract or a dried object, this dried object can pass through drying
Extract obtained by step (c) and provide., optionally, can be in progress step (b) to reach maximum extraction benefit as far as possible
Before, Poria cocos skin zone is repeated to extract with the first identical or different polar solvent, and merged obtained by the multiple extraction
Extract carries out the thick extraction thing of step (b) to provide；Also may be repeated step (b), step (c) and it is foregoing optionally
The circulation of other operations.
In according in Poria cocos skin zone of the present invention extract, with the gross weight meter of Poria cocos skin zone extract, Poria cocos
Eo-acid A and Poria cocos eo-acid B total content are not less than 30 weight %, are preferably not less than 40 weight %, and pachymic acid, dehydrogenation Poria cocos
Acid, each content of dehydrotumulosic acid are not all no more than 0.5% for acid, soil, dehydrogenation bolt bacterium acid, bolt bacterium acid, dehydrogenation shelf fungus acid, layer
Each content of pore fungi acid is all no more than 5%.It is preferred that in the Poria cocos skin zone extract, with the total of Poria cocos skin zone extract
Weight meter, dehydrogenation bolt bacterium acid, bolt bacterium acid, dehydrogenation shelf fungus acid, each content of shelf fungus acid are all no more than 2.5%.More preferably,
In the Poria cocos skin zone extract, with the gross weight meter of Poria cocos skin zone extract, dehydrogenation bolt bacterium acid, bolt bacterium acid, dehydrogenation shelf fungus
Acid, each content of shelf fungus acid are all no more than 1%.
In the medical composition or medicine that application according to the present invention is provided can in it is any it is suitable in the form of, it is special to have no
Limitation, end regard desired purposes and are in corresponding suitable dosage form.For example, but it is not limited, the medical composition or medicine
Thing can it is oral or it is non-by oral administration (such as：Subcutaneously, intravenously, muscle or abdominal cavity) dosing mode be applied in need
On body.Wherein, depending on type of service and purposes, suitable supporting agent can be selected to provide the medical composition or medicine, wherein,
The supporting agent includes excipient, diluent, adjuvant, stabilization agent, absorption delaying agent, disintegrating agent, solubilizer, emulsifying agent, anti-oxidant
Agent, binder, bonding agent, tackifier, dispersant, suspending agent, lubricant, hygroscopic agent etc..
It is suitable for exemplified by oral dosage form, the medical composition or medicine provided in application according to the present invention can contain
Any benefit that is intended to for adversely influenceing active component (that is, Poria cocos eo-acid A, Poria cocos eo-acid B or Poria cocos skin zone extract)
Pharmaceutically acceptable supporting agent, such as：Water, saline solution, glucose (dextrose), glycerine, ethanol or its analog, fiber
Element, starch, sugared bentonite (sugarbentonite) and foregoing combination.Using any suitable method, it is suitable for oral
The dosage form of dispensing provides the medical composition or medicine, such as：Lozenge (such as sugar-coat ingot), pill, capsule, granule, dissipate
Agent, liquid extract, solution, syrup, suspension agent, tincture etc..
, then can be according to the present invention's as the injection suitable for subcutaneous, intravenous, muscle or intraperitoneal injection or point drops
Using containing one or more such as isotonic solutions, salt buffer solution (such as phosphate in the medical composition or medicine provided
Buffer solution or citrate buffer), solubilizer, emulsifying agent, the composition such as 5% sugar juice and other supporting agents, with venoclysis
The dosage forms such as liquid, emulsion venoclysis liquid, dry powder injection, suspension injection or dry powder suspension injection provide the medicinal combination
Thing or medicine.Or can be by the medical composition or medicine preparation into solid before an injection, to dissolve in other solution or suspension
Dosage form or emulsifiable dosage form in liquid provide solid before the injection, and in administering to before individual in need, this is injected
Preceding solid is dissolved in other solution or suspension or is emulsified, there is provided desired injection.
Optionally, suitable use can be contained in addition in the medical composition or medicine that application according to the present invention is provided
The additive of amount, such as the flavor enhancement of the suitable sense of the mouth of the medical composition or medicine when taking and visual experience can be improved, adjusted
Toner, colouring agent etc., and can improve the stability of the medicine and the buffer of storage characteristics, preservative agent, preservative, antiseptic,
Antifungal agent etc..In addition, the medical composition or medicine can be optionally (such as anti-containing one or more other active components in addition
Oxidant, insulin sensitizer etc.), or with the drug combination containing one or more other active components, with further plus
The effect of strong medical composition or medicine or the use flexibly and allotment degree of increase pharmaceutical formulation, if this other it is active into
Divide does not have unfavorable shadow to the benefit of inventive compound (that is, Poria cocos eo-acid A, Poria cocos eo-acid B or Poria cocos skin zone extract)
Sound.
The medical composition or medicine provided in application according to the present invention can once a day, one day repeatedly or number
Day one, inferior different dosing frequencies were applied, and end is different regarding administering individual demand, age, body weight and healthy condition shape.Citing speech
It, is when being applied to an individual with oral way to adjust blood glucose, with Poria cocos eo-acid A and Poria cocos eo-acid B gross weight meter, its
Dosage is daily about 0.01 mg kg of body weight to 5 mg kg of body weight, and preferably daily about 0.03 mg kg of body weight is extremely
2 mg kg of body weight, it is more preferably daily about 0.05 mg kg of body weight to 1 mg kg of body weight.Or with Poria cocos skin zone
Extract meter, its dosage are daily about 0.025 mg kg of body weight to 25 mg kg of body weight, preferably daily about 0.075
Mg kg of body weight to 10 mg kg of body weight, be more preferably daily about 0.125 mg kg of body weight to 5 mgs/kg of bodies
Weight.
The food that application according to the present invention is provided can be health food, nutrient supplement food or special dietary food
Product, and such as dairy products, meat packing product, Bread and Pastries, pastries, biscuit, mouth containing ingot, capsule, juice, tea can be made
The products such as class, sports drink, nutritious drink, but be not limited.It is preferred that the food of application according to the present invention is eaten with health care
The form of product provides.
Health food, nutrient supplement food and the food of special nutrients provided in application according to the present invention can be with one day
Once, repeatedly or one inferior different frequency of a few days is eaten end regarded administering individual age, body weight and health status and adopted on 1st
It is recommended that intake and it is different.Also can be directed to specific group adjust health food provided by the present invention, nutrient supplement food and
The content of Poria cocos eo-acid A, Poria cocos eo-acid B or Poria cocos skin zone extract in food of special nutrients, preferably adjust to should take daily
Amount.For example, with Poria cocos eo-acid A and Poria cocos eo-acid B gross weight meter, if the suggestion intake of an individual is daily
The Poria cocos eo-acid A and Poria cocos eo-acid B that total amount is about 70 milligrams, but every part of the health food is containing the Poria cocos eo-acid that total amount is 35 milligrams
A and Poria cocos eo-acid B, then daily about two portions of health foods of edible of the individual.
It can suggest using in the outer packing sign of health food of the present invention, nutrient supplement food and/or food of special nutrients
Amount, the use standard of specific group (such as pregnant woman, diabetic, Patients With Kidney Diseases) and condition or with other food or doctor
The suggestion item that medicine is taken jointly, voluntarily taken so that user can be in the case where being instructed without doctor, pharmacist or relevant staff
With and without security concerns.
The present invention also provides a kind of method for adjusting blood glucose, and it includes the work that individual in need to one applies an effective dose
Property composition, the wherein active component is at least one of Poria cocos eo-acid A and Poria cocos eo-acid B.In the regulation blood glucose according to the present invention
Method in, the application of the aspect about the active component, administering approach, administering form, suitable dose and associated treatment,
As the above description.
The present invention is further now illustrated with the following example.Wherein these embodiments are merely provided as illustrating, rather than
To limit the scope of the invention.The scope of the present invention is as shown in claims.
Embodiment
[preparation embodiment]
A. the preparation of Poria cocos skin zone extract
A-1. Poria cocos medicinal material (the source place of production is Yunnan) is taken, its crust (calling in the following text " Poria cocos skin zone ") is stripped after cleaning, remaining
As meat portion (calling in the following text in " Poria cocos meat portion ").Foregoing Poria cocos skin zone is taken, at room temperature, with 1：8 (Poria cocos medicinal materials：Ethanol water)
Volume ratio be soaked in 75% ethanol water, last 12 hours, then boil and extracted and (last 3 hours).Repeat
Foregoing extraction step, altogether three times.Merge the extract of extraction gained three times and filter to remove insoluble matter, to obtain a slightly extraction
Thing.Then, foregoing thick extract is concentrated under reduced pressure to remove solvent, then be dried with spray dryer, to obtain
One thick extraction thing powder.
A-2. the thick extraction thing powder that A-1 is obtained is taken, with 1：8 (thick extraction thing powder：Ethanol water) volume ratio with
95% ethanol mixes, and is extracted and (last 3 hours), then, recycles the tubing string using silica gel as stationary phase to be separated, obtains
Obtain a Poria cocos skin zone extract.
A-3. the thick extraction thing powder that A-1 is obtained is taken, with 1：10 (thick extraction thing powder：Water) volume ratio be dispersed in it is pure
In water.Then, adding sodium hydroxide makes the pH value of the mixture be lifted to about 12, then pours into the modulation bucket that temperature is maintained at 65 DEG C
In and uniform stirring until reaction is complete.Then, neutralized with 12N concentrated hydrochloric acid, filtrate is removed after centrifugation, and it is clear with pure water
Remaining insoluble matter is washed, then insoluble matter is dried with spray dryer, obtains an extract powder.Take foregoing extract
Powder, with 1：20 (extract powder：1N sodium bicarbonate aqueous solutions) volume ratio, use 1N sodium bicarbonate aqueous solutions extraction three
It is secondary, merge the extract of extraction gained three times, neutralized with 12N concentrated hydrochloric acid, filtrate is removed after centrifugation, and clean with pure water
Remaining insoluble matter, then insoluble matter is dried with spray dryer, obtain a Poria cocos skin zone extract.
A-4. with liquid chromatography/ultraviolet light/mass spectrograph, respectively at detection A-2, A-3 under 243 nms and 210 nm wavelength
The composition of the extract obtained, and with high performance liquid chromatography quantitatively respectively in the extract each composition content, wherein, by A-
The analysis result of 2 extracts obtained is shown in table 1, the analysis result for the extract that A-3 is obtained is shown in table 2.
Table 1
Table 2
| Composition | Weight % |
| Pachymic acid (pachymic acid, PA) | - |
| DHPA (dehydropachymic acid, DPA) | - |
| Soil is not sour (tumulosic acid, TA) | - |
| Dehydrotumulosic acid (dehydrotumulosic acid, DTA) | 0.31 |
| Umbellate pore furgus acid C (Polyporenic acid C, PAC) | 1.15 |
| 3- tables-dehydrotumulosic acid (3-epi-dehydrotumulosic acid, EDTA) | 0.40 |
| Dehydrogenation bolt bacterium acid (dehydrotrametenolic acid, DTTA) | 0.58 |
| Bolt bacterium acid (trametenolic acid, TTA) | 0.35 |
| Poria cocos eo-acid A (poricoic acid A, PAA) | 41.06 |
| Dehydrogenation shelf fungus acid (dehydroeburicoic acid, DEA) | 0.19 |
| Poria cocos eo-acid B (poricoic acid B, PAB) | 16.50 |
| Shelf fungus acid (eburicoic acid, EA) | 0.20 |
As shown in Table 1, the Poria cocos eo-acid A that the Poria cocos skin zone extract that A-2 is obtained contains a large amount is (in the weight of extract
Measure percentage for 32.72%) with Poria cocos eo-acid B (in the percentage by weight of extract be 10.44%), the dehydrogenation bolt bacterium of low amounts
Acid, bolt bacterium acid, dehydrogenation shelf fungus acid and shelf fungus acid (in the percentage by weight of extract be respectively 2.01%, 0.85%,
1.2%th, 0.83%) and much lower amounts dehydrotumulosic acid (in the percentage by weight of extract be 0.46%), but be free of Fu
Siberian cocklebur acid, DHPA and soil is not sour.
As shown in Table 2, the Poria cocos eo-acid A that the Poria cocos skin zone extract that A-3 is obtained contains a large amount is (in the weight of extract
Percentage be 41.06%) with Poria cocos eo-acid B (in the percentage by weight of extract be 16.50%), umbellate pore furgus acid C, the dehydrogenation of low amounts
Bolt bacterium acid (in the percentage by weight of extract be respectively 1.15%, 0.58%) and much lower amounts dehydrotumulosic acid, 3-
Table-dehydrotumulosic acid, bolt bacterium acid, dehydrogenation shelf fungus acid and shelf fungus acid (in the percentage by weight of extract be respectively 0.31%,
0.40%th, 0.35%, 0.19%, 0.20%), it is but not sour without pachymic acid, DHPA and soil.
B. Poria cocos eo-acid A and Poria cocos eo-acid B preparation
B-1. with 1：500 (Poria cocos skin zone extracts：Methanol) volume ratio, make the Poria cocos skin zone extraction that A-2 or A-3 obtained
Thing uniform dissolution is taken in methanol.Filter off after removing insoluble matter, (mixed with the high-effect liquid chromatograph of preparation scale with methanol with water
As mobile phase), under 243 nm wavelength, separated and collected for Poria cocos eo-acid A and Poria cocos eo-acid B, after collection again with
The machine that is concentrated under reduced pressure removes methanol, respectively obtains Poria cocos eo-acid A and Poria cocos eo-acid B.
B-2. it is new respectively at the Poria cocos that detection B-1 is obtained under 243 nm wavelength with liquid chromatography/ultraviolet light/mass spectrograph
Sour A and Poria cocos eo-acid B, as a result show that Poria cocos eo-acid A and Poria cocos eo-acid B purity is all more than 98%.
C. cell culture
The mouse muscle cell (C2C12, purchased from ATCC) completed and adipocyte (3T3-L1, purchased from ATCC) point will be broken up
Do not cultivate in the Du Shi improved culture mediums containing 2% bovine serum albumin (BSA) but without serum (serum-free)
In (Dulbecco's modified Eagle's medium, DMEM), 16 hours are lasted.Then, with Du Shi phosphate-buffereds
Liquid (Dulbecco's phosphate-bufferedsaline, D-PBS) cleans, and culture medium is replaced by micro- containing 500
The 0.2%BSA-DMEM culture mediums of grams per milliliter glucose, so that subsequent experimental uses.
Embodiment 1：Influence of the Poria cocos skin zone extract to cellular uptake glucose ability
(1-1) muscle cell
The C2C12 cells for taking [preparation embodiment] to be provided, it is divided into five groups and is trained respectively with following culture medium
Support, last 2 hours：
1. Group I：BSA-DMEM culture mediums containing 500 microgram glucose/milliliter；
2. Group II：Containing 500 microgram glucose/milliliter and concentration be 100 how the BSA- of the insulin of mole concentration
DMEM culture mediums；
3. Group III：Containing 500 microgram glucose/milliliter and concentration [embodiment is prepared for 0.1 mcg/ml
A-2] the BSA-DMEM culture mediums of Poria cocos skin zone extract solution that are provided；
4. Group IV：Contain [the preparing embodiment A-2] that 500 microgram glucose/milliliter and concentration are 1 mcg/ml
The BSA-DMEM culture mediums of the Poria cocos skin zone extract solution provided；
5. Group V：Contain [the preparing embodiment A-2] that 500 microgram glucose/milliliter and concentration are 10 mcg/mls
The BSA-DMEM culture mediums of the Poria cocos skin zone extract solution provided.
Thereafter, with the glucose content in the glycoxidative ferment method measure each group cell culture fluid of grape, to understand each group
Glucose consumption degree (ability for representing cellular uptake glucose).Finally, with control group (that is, with Group I nutrient solution culture
Cell) result on the basis of, calculate other each groups versus glucose intake ability, be as a result shown in Fig. 1.
As shown in Figure 1, compared to control group, cell through Poria cocos skin zone of the present invention extract processing (that is, with III,
The cell of IV or V tissue culture nutrient solution cultures) glucose uptake ability be obviously improved, or even surmount positive control group (that is, with II
The cell of tissue culture nutrient solution culture).Aforementioned result shows that Poria cocos skin zone of the present invention extract can effectively lift muscle cell intake Portugal
The ability of grape sugar, therefore can be used for adjusting blood glucose.
(1-2) adipocyte
The 3T3-L1 cells for taking [preparation embodiment] to be provided, it is divided into five groups and respectively with embodiment 1 (1-1) Suo Shu
I to V group culture mediums cultivated, last 2 hours.Then, with the glycoxidative ferment method measure each group cell culture fluid of grape
In glucose content, to understand the glucose consumption degree of each group (ability for representing cellular uptake glucose).Finally, with control
On the basis of the result of processed group (that is, by the cell of Group I nutrient solution culture), the versus glucose intake energy of other each groups is calculated
Power, as a result it is shown in Fig. 2.
As shown in Figure 2, compared to control group, cell through Poria cocos skin zone of the present invention extract processing (that is, with III,
The cell of IV or V tissue culture nutrient solution cultures) glucose uptake ability all have the trend of rising, wherein, with high dose group (with V
The cell of tissue culture nutrient solution culture) ascendant trend it is the most notable.Aforementioned result shows that Poria cocos skin zone of the present invention extract can be effective
The ability of adipocyte intake glucose is lifted, therefore can be used for adjusting blood glucose.
Embodiment 2：The influence of Poria cocos eo-acid A and Poria cocos eo-acid B to cellular uptake glucose ability
(2-1) muscle cell
The C2C12 cells for taking [preparation embodiment] to be provided, it is divided into eight groups and is trained respectively with following culture medium
Support, last 2 hours：
1. i-th group：BSA-DMEM culture mediums containing 500 microgram glucose/milliliter；
2. the i-th i groups：Containing 500 microgram glucose/milliliter and concentration be 100 how the BSA- of the insulin of mole concentration
DMEM culture mediums；
3. the i-th ii groups：Containing 500 microgram glucose/milliliter and concentration [embodiment is prepared for 0.1 mcg/ml
B-1] the Poria cocos eo-acid A that is provided or Poria cocos eo-acid B BSA-DMEM culture mediums；
4. the i-th v groups：Contain [the preparing embodiment B-1] that 500 microgram glucose/milliliter and concentration are 1 mcg/ml
The Poria cocos eo-acid A (or Poria cocos eo-acid B) provided BSA-DMEM culture mediums；
5. v groups：Contain [the preparing embodiment B-1] that 500 mcg/ml glucose and concentration are 10 mcg/mls
The Poria cocos eo-acid A (or Poria cocos eo-acid B) provided BSA-DMEM culture mediums.
Then, with the content of glucose in the glycoxidative ferment method measure each group cell culture fluid of grape, to understand each group
Glucose consumption degree (ability for representing cellular uptake glucose), finally, with control group (that is, with the i-th tissue culture nutrient solution culture
Cell) result on the basis of, calculate other each groups versus glucose intake ability, be as a result shown in Fig. 3 A and Fig. 3 B.Wherein, scheme
3A includes control group, positive control group (that is, with the cell of the i-th i tissue culture nutrient solution cultures) and the group handled through Poria cocos eo-acid A
The result of (that is, Poria cocos eo-acid A being contained with the cell of i-th ii, iv or v tissue culture nutrient solution culture, the wherein nutrient solution).Fig. 3 B are then
Comprising control group, positive control group and through Poria cocos eo-acid B handle group (that is, with the thin of i-th ii, iv or v tissue culture nutrient solution culture
Born of the same parents, the wherein nutrient solution contain Poria cocos eo-acid B) result.
From Fig. 3 A, compared to control group, the glucose uptake ability of the group handled through Poria cocos eo-acid A is obviously improved
It is extremely suitable with positive control group.Aforementioned result shows that Poria cocos eo-acid A can effectively lift the ability of muscle cell intake glucose, therefore
Available for adjusting blood glucose.
From Fig. 3 B, compared to control group, the glucose uptake ability of the group handled through Poria cocos eo-acid B also significantly carries
Rise.Aforementioned result shows that Poria cocos eo-acid B also can adjust blood glucose by lifting the ability of muscle cell intake glucose.
(2-2) adipocyte
The 3T3-L1 cells for taking [preparation embodiment] to be provided, it is divided into eight groups and respectively with embodiment 2 (2-1) Suo Shu
I-th cultivated to v group culture mediums, last 2 hours.Then, with the glycoxidative ferment method measure each group cell culture fluid of grape
In glucose content, to understand the glucose consumption degree of each group (ability for representing cellular uptake glucose).Finally, with control
On the basis of the result of processed group (that is, by the cell of the i-th tissue culture nutrient solution culture), the versus glucose intake energy of other each groups is calculated
Power, as a result it is shown in Fig. 4 A and Fig. 4 B.Wherein, Fig. 4 A include control group, positive control group (that is, with the thin of the i-th i tissue culture nutrient solution cultures
Born of the same parents) and through Poria cocos eo-acid A handle group (that is, with the i-th i i, the wherein cell of iv or v tissue culture nutrient solution cultures, the nutrient solution
Contain Poria cocos eo-acid A) result.Fig. 4 B then comprising control group, positive control group and through Poria cocos eo-acid B handle group (that is, with
The cell of i-th ii, iv or v tissue culture nutrient solution culture, the wherein nutrient solution contain Poria cocos eo-acid B) result.
From Fig. 4 A, compared to control group, the glucose uptake ability of the group handled through Poria cocos eo-acid A has rising
Trend, wherein, with middle dose group (that is, with the cell of the i-th v tissue culture nutrient solution cultures) and high dose group (that is, with v tissue culture nutrient solutions
The cell of culture) ascendant trend be notable.Aforementioned result shows that Poria cocos eo-acid A can effectively lift adipocyte intake grape
The ability of sugar, therefore can be used for adjusting blood glucose.
From Fig. 4 B, compared to control group, the glucose uptake ability of the group handled through Poria cocos eo-acid B significantly carries
Rise.Aforementioned result shows that Poria cocos eo-acid B also can adjust blood glucose by lifting the ability of adipocyte intake glucose.
As shown in above-mentioned embodiment, Poria cocos skin zone of the present invention extract and Poria cocos eo-acid A and Poria cocos eo-acid B can be carried really
The ability of biological cell intake blood glucose is risen, available for adjusting blood glucose, and especially can reduce too high blood glucose.
Claims (13)
1. one kind uses at least the one of Poria cocos eo-acid A (poricoic acid A) and Poria cocos eo-acid B (poricoic acid B)
The individual purposes in one medicine of manufacture or food, it is characterised in that the medicine or food are used to adjust blood glucose.
2. purposes as claimed in claim 1, it is characterised in that Poria cocos eo-acid A and Poria cocos eo-acid B at least one being extracted with plant
The form of thing is taken to use.
3. purposes as claimed in claim 2, it is characterised in that with the gross weight meter of plant extract, Poria cocos eo-acid A and Poria cocos
Eo-acid B total content is not less than 30 weight %.
4. purposes as claimed in claim 3, it is characterised in that with the gross weight meter of plant extract, Poria cocos eo-acid A and Poria cocos
Eo-acid B total content is not less than 40 weight %.
5. the purposes as any one of claim 2 to 4, it is characterised in that the plant extract is the extraction of Poria cocos skin zone
Thing.
6. purposes as claimed in claim 5, it is characterised in that with the gross weight meter of Poria cocos skin zone extract, pachymic acid
(pachymic acid), DHPA (dehydropachymic acid), soil not sour (tumulosic acid) and go
Each content of hydrogen soil not sour (dehydrotumulosic acid) is all no more than 0.5%.
7. purposes as claimed in claim 5, it is characterised in that with the gross weight meter of Poria cocos skin zone extract, dehydrogenation bolt bacterium acid
(dehydrotrametenolic acid), bolt bacterium acid (trametenolic acid), dehydrogenation shelf fungus acid
Each content of (dehydroeburicoic acid), shelf fungus acid (eburicoic acid) is all no more than 5%.
8. purposes as claimed in claim 7, it is characterised in that with the gross weight meter of Poria cocos skin zone extract, dehydrogenation bolt bacterium acid,
Bolt bacterium acid, dehydrogenation shelf fungus acid, each content of shelf fungus acid are all no more than 2.5%.
9. purposes as claimed in claim 8, it is characterised in that with the gross weight meter of Poria cocos skin zone extract, dehydrogenation bolt bacterium acid,
Bolt bacterium acid, dehydrogenation shelf fungus acid, each content of shelf fungus acid are all no more than 1%.
10. purposes as claimed in claim 5, it is characterised in that the operation of the Poria cocos skin zone extract to comprise the following steps
There is provided：
(a) with the Poria cocos skin zone of one first solvent extraction one, obtain one and slightly extract thing；
(b) the thick extraction thing is dried, one is obtained and slightly extracts thing powder；
(c) thick extraction thing powder with one second solvent extraction, obtains a Poria cocos skin zone extract,
Wherein, first solvent and second solvent are identical or different and are respectively selected from water, ethanol, alkali lye, acid solution and foregoing
Combination.
11. purposes as claimed in claim 10, it is characterised in that first solvent is that concentration of alcohol is identical with the second solvent
Or different ethanol water.
12. purposes as claimed in claim 1, it is characterised in that with Poria cocos eo-acid A and Poria cocos eo-acid B gross weight meter, the medicine
The dosage of thing or food is daily about 0.05 mg kg of body weight to 1 mg kg of body weight.
13. purposes as claimed in claim 1, it is characterised in that the food is health food, nutrient supplement food or special battalion
Support food.
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| CN202211163103.0A CN115536522A (en) | 2016-05-10 | 2017-05-09 | Use of pachyman cortex extract, pachyman neo-acid A and pachyman neo-acid B for regulating blood sugar |
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| CN202211163103.0A Pending CN115536522A (en) | 2016-05-10 | 2017-05-09 | Use of pachyman cortex extract, pachyman neo-acid A and pachyman neo-acid B for regulating blood sugar |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH10330266A (en) * | 1997-06-02 | 1998-12-15 | Kotarou Kanpo Seiyaku Kk | Composition having insulin action-enhancing activity |
| CN104688782A (en) * | 2015-02-05 | 2015-06-10 | 广东药学院 | Method for efficiently extracting triterpene active components from Indian buead peel |
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| JP2005089328A (en) * | 2003-09-12 | 2005-04-07 | Univ Nihon | Dna synthesizing enzyme- and dna topoisomerase-inhibiting composition |
| CN103550265B (en) * | 2013-11-08 | 2015-07-01 | 山东省中医药研究院 | Extraction method of active ingredients of tuckahoe peels and tuckahoe peel extracts |
-
2017
- 2017-05-09 CN CN201710320602.9A patent/CN107349192A/en active Pending
- 2017-05-09 CN CN202211163103.0A patent/CN115536522A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH10330266A (en) * | 1997-06-02 | 1998-12-15 | Kotarou Kanpo Seiyaku Kk | Composition having insulin action-enhancing activity |
| CN104688782A (en) * | 2015-02-05 | 2015-06-10 | 广东药学院 | Method for efficiently extracting triterpene active components from Indian buead peel |
Non-Patent Citations (3)
| Title |
|---|
| MAYUMI SATO ET AL: "Dehydrotrametenolic Acid Induces Preadipocyte Differentiation and Sensitizes Animal Models of Noninsulin-Dependent Diabetes Mellitus to Insulin", 《BIOLOGICAL PHARMACEUTICAL BULLETIN》 * |
| 仲兆金等: "茯苓有效成分三萜的研究进展", 《中成药》 * |
| 董文远: "茯苓中三萜的分离纯化及含量测定研究", 《中国优秀博硕士学位论文全文数据库（硕士）医药卫生科技辑》 * |
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Application publication date: 20171117 |
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| RJ01 | Rejection of invention patent application after publication |